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TargetSerine/threonine-protein kinase PLK1
LigandBDBM50343561
Substrate/Competitorn/a
Meas. Tech.ChEMBL_747145 (CHEMBL1777511)
IC50 43±n/a nM
Citation Beria, IBossi, RTBrasca, MGCaruso, MCeccarelli, WFachin, GFasolini, MForte, BFiorentini, FPesenti, EPezzetta, DPosteri, HScolaro, ARe Depaolini, SValsasina, B NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett21:2969-74 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Serine/threonine-protein kinase PLK1
Name:Serine/threonine-protein kinase PLK1
Synonyms:PLK | PLK-1 | PLK1 | PLK1_HUMAN | Polo-like kinase 1 (PlK1) | Polo-like kinase 1 (Plk-1) | STPK13 | Serine/threonine-protein kinase (PLK1) | Serine/threonine-protein kinase 13 | polo-like kinase
Type:Serine/threonine-protein kinase
Mol. Mass.:68277.16
Organism:Homo sapiens (Human)
Description:P53350
Residue:603
Sequence:
MSAAVTAGKLARAPADPGKAGVPGVAAPGAPAAAPPAKEIPEVLVDPRSRRRYVRGRFLG
KGGFAKCFEISDADTKEVFAGKIVPKSLLLKPHQREKMSMEISIHRSLAHQHVVGFHGFF
EDNDFVFVVLELCRRRSLLELHKRRKALTEPEARYYLRQIVLGCQYLHRNRVIHRDLKLG
NLFLNEDLEVKIGDFGLATKVEYDGERKKTLCGTPNYIAPEVLSKKGHSFEVDVWSIGCI
MYTLLVGKPPFETSCLKETYLRIKKNEYSIPKHINPVAASLIQKMLQTDPTARPTINELL
NDEFFTSGYIPARLPITCLTIPPRFSIAPSSLDPSNRKPLTVLNKGLENPLPERPREKEE
PVVRETGEVVDCHLSDMLQQLHSVNASKPSERGLVRQEEAEDPACIPIFWVSKWVDYSDK
YGLGYQLCDNSVGVLFNDSTRLILYNDGDSLQYIERDGTESYLTVSSHPNSLMKKITLLK
YFRNYMSEHLLKAGANITPREGDELARLPYLRTWFRTRSAIILHLSNGSVQINFFQDHTK
LILCPLMAAVTYIDEKRDFRTYRLSLLEEYGCCKELASRLRYARTMVDKLLSSRSASNRL
KAS
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BDBM50343561
n/a
NameBDBM50343561
Synonyms:8-(5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenylamino)-1-(2-(tetrahydro-2H-pyran-4-yloxy)ethyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1774338
TypeSmall organic molecule
Emp. Form.C29H35F3N8O4
Mol. Mass.616.6346
SMILESCN1CCN(CC1)c1ccc(OC(F)(F)F)c(Nc2ncc3CCc4c(nn(CCOC5CCOCC5)c4-c3n2)C(N)=O)c1
Structure
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